The present invention relates to novel templates useful for generating novel compounds and to compounds produced utilizing the templates. The templates comprise quaternary amino acids that may be linked to solid supports. These templates make possible the production of novel classes of chemical compounds through a plurality of chemical reactions. The templates are advantageous for use in drug discovery regimes.
The use of solid phase synthesis techniques for the synthesis of polypeptides and oligonucleotides is known. More recently, the use of solid phase techniques for the synthesis of small organic molecules has become a major focus of research. Of prime importance has been the ability of solid phase techniques to be automated, with an attendant increase in compound throughput and efficiency in research. This has been exploited with great vigor in the area of pharmaceutical research where it has been estimated that 10,000 compounds must be synthesized and tested in order to find one new drug (Science 259:1564, (1993)). The focus on combinatorial chemistry techniques to increase compound throughput has now become almost universal in the pharmaceutical and agricultural industries.
An additional aspect of combinatorial chemistry relates to the chemical diversity of the compound stocks that are available for screening by the pharmaceutical companies in the search for new lead structures. These have tended to be limited to the classes of compounds previously investigated through medicinal chemical techniques within each company. Therefore, the availability of new classes of molecules for screening has become a major need.
As a consequence of the development of efficient automation equipment and processes, parallel synthesis techniques have become the most extensively used method in combinatorial chemistry. The field of pharmaceutical and agricultural research has a strong need for highly flexible technologies and chemical building blocks with and without the polymer support to generate a large number of novel classes of compounds for screening and clinical testing.
Thus, templates such as those presented in the present invention are highly desirable and valuable, in particular in the synthesis of peptides and of amino acid containing compounds for drug discovery.
The present invention provides support templates that may be utilized to generate novel compounds. The support templates comprise amino acids that may be linked to polymeric supports to form a platform for chemical discovery.
In general terms the present invention provides quaternary amino acids that are capable of being used as templates for the synthesis of other molecules including peptides, other amino acids, and other compounds that may be useful in pharmaceutical, agricultural, food product and/or related settings. The quaternary amino acids may be linked to a solid support to form a template that may be utilized in solid phase synthesis techniques that advantageously permit compounds with intermediates relatively unstable to other techniques to be synthesized and isolated. Embodiments of the present invention may be utilized in combinatorial chemistry using parallel synthesis techniques to create and screen large libraries of potentially useful compounds.
Details and embodiments of the present invention are set forth below and in the appended drawings.